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Synthesis and Antimycobacterial and Photosynthesis-Inhibiting Evaluation of 2-[(E)-2-Substituted-ethenyl]-1,3-benzoxazoles

التفاصيل البيبلوغرافية
العنوان: Synthesis and Antimycobacterial and Photosynthesis-Inhibiting Evaluation of 2-[(E)-2-Substituted-ethenyl]-1,3-benzoxazoles
المؤلفون: Ales Imramovsky, Jan Kozic, Matus Pesko, Jirina Stolarikova, Jarmila Vinsova, Katarina Kralova, Josef Jampilek
المصدر: The Scientific World Journal, Vol 2014 (2014)
بيانات النشر: Wiley, 2014.
سنة النشر: 2014
المجموعة: LCC:Technology
LCC:Medicine
LCC:Science
مصطلحات موضوعية: Technology, Medicine, Science
الوصف: A series of twelve 2-[(E)-2-substituted-ethenyl]-1,3-benzoxazoles was designed. All the synthesized compounds were tested against three mycobacterial strains. The compounds were also evaluated for their ability to inhibit photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. 2-[(E)-2-(4-Methoxyphenyl)ethenyl]-1,3-benzoxazole, 2-[(E)-2-(2,3-dihydro-1-benzofuran-5-yl)ethenyl]-1,3-benzoxazole and 2-{(E)-2-[4-(methylsulfanyl)phenyl]ethenyl}-1,3-benzoxazole showed the highest activity against M. tuberculosis, M. kansasii, and M. avium, and they demonstrated significantly higher activity against M. avium and M. kansasii than isoniazid. The PET-inhibiting activity of the most active ortho-substituted compound 2-[(E)-2-(2-methoxyphenyl)ethenyl]-1,3-benzoxazole was IC50 = 76.3 μmol/L, while the PET-inhibiting activity of para-substituted compounds was significantly lower. The site of inhibitory action of tested compounds is situated on the donor side of photosystem II. The structure-activity relationships are discussed.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 2356-6140
1537-744X
Relation: https://doaj.org/toc/2356-6140; https://doaj.org/toc/1537-744X
DOI: 10.1155/2014/705973
URL الوصول: https://doaj.org/article/e08858e23c2e434180910b467a38d516
رقم الأكسشن: edsdoj.08858e23c2e434180910b467a38d516
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:23566140
1537744X
DOI:10.1155/2014/705973